[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) › Darolutamide # Darolutamide ## Antiandrogens and androgen synthesis inhibitors? Antiandrogens and androgen synthesis inhibitors ## Pregnancy: contraindicated? Contraindicated in women who are or may become pregnant (EU label). Darolutamide is for men only; it can harm a fetus, and men use contraception with a partner who could conceive… An oral androgen receptor blocker for prostate cancer, used with ongoing testosterone suppression. Taken with food. Updated Nov 12, 2026 ## Quick facts **Group** [Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) **Target** Androgen receptor (AR) **Key effects** Fatigue · Pain in the arms or legs · Rash **Monitor** PSA and imaging for response · Blood pressure **ATC** L02BB06 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Clinical What the labels mean - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ◎**Androgen receptor (AR)**Darolutamide ⓘ No crystal structure with darolutamide is available. The figure shows bicalutamide, an older antiandrogen, in the same ligand-binding pocket of the human androgen receptor. **Target in 3D:** Androgen receptor (AR). PDB structure 1Z95 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/1Z95) · Drag to rotate · pinch to zoom Darolutamide binds the ligand-binding domain of the androgen receptor and blocks testosterone and dihydrotestosterone. It also stops the receptor from moving into the nucleus and switching on androgen-driven genes, so prostate cancer cells stop growing. It is given together with treatment that keeps testosterone low. - Binds the androgen receptor ligand pocket - Blocks nuclear entry and gene activation - Androgen-driven prostate cancer stops growing ## Indications - Non-metastatic castration-resistant prostate cancer. [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) - Metastatic hormone-sensitive prostate cancer, alone or with docetaxel. [Prostate cancer →](https://durgical.com/en/conditions/prostate-cancer/) ## Adverse effects ### Common - Fatigue - Pain in the arms or legs - Rash ### Serious (rare, important) - Seizures - Heart problems: chest pain, heart failure - Blood in the urine ## Contraindications - Hypersensitivity to darolutamide - Pregnancy (EU label) ## Key interactions **St John's wort** Can lower darolutamide levels; reviewed before starting. **Grapefruit and its juice** Can change darolutamide levels; avoided. **GnRH analogues (leuprorelin, goserelin, triptorelin)** Continued alongside: darolutamide works on top of testosterone suppression. ## What is monitored - PSA and imaging for response - Blood pressure and cardiovascular risk factors - Liver tests - Rash and seizures ## Administration and safety - Oral tablets swallowed whole with food, not split, crushed or chewed. - Testosterone-lowering treatment continues during darolutamide. ## Pregnancy and breastfeeding Contraindicated in women who are or may become pregnant (EU label). Darolutamide is for men only; it can harm a fetus, and men use contraception with a partner who could conceive during treatment and for a week after. ## Nursing care - Teach to take it with food and not to stop the GnRH analogue. - Teach to avoid grapefruit and St John's wort. - Teach to report chest pain, seizures, rash or blood in the urine. - Men with a partner who could conceive use contraception during treatment and shortly after. ## Pharmacokinetics **Absorption** Oral tablets twice a day with food. ## Memory aid «-lutamide blocks the lock»: darolutamide, apalutamide and enzalutamide all fill the androgen receptor's lock. ## Test yourself Think of the answer, then tap the question to see it. ## What is the target of darolutamide? The androgen receptor (ligand-binding domain). ## Which treatment must continue during darolutamide? Testosterone suppression with a GnRH analogue or orchiectomy. ## With which chemotherapy is darolutamide combined in metastatic hormone-sensitive disease? Docetaxel. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/darolutamide/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## What the labels mean **Pregnancy: contraindicated** Contraindicated in women who are or may become pregnant (EU label). Darolutamide is for men only; it can harm a fetus, and men use contraception with a partner who could conceive… ## Connections ## Related drugs 3 - [Apalutamide](https://durgical.com/en/pharmacology/apalutamide/) - [Enzalutamide](https://durgical.com/en/pharmacology/enzalutamide/) - [Abiraterone](https://durgical.com/en/pharmacology/abiraterone/) ## Related conditions 1 - [Prostate cancer](https://durgical.com/en/conditions/prostate-cancer/) [← Back to the class: Antiandrogens and androgen synthesis inhibitors](https://durgical.com/en/pharmacology/classes/antiandrogens-and-androgen-synthesis-inhibitors/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [Darolutamide: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a619045.html) (MedlinePlus (U.S. National Library of Medicine), 2022); [Darolutamide - NCI](https://www.cancer.gov/about-cancer/treatment/drugs/darolutamide) (National Cancer Institute, 2026); [EMA: product information for darolutamide](https://www.ema.europa.eu/en/documents/product-information/nubeqa-epar-product-information_en.pdf) (European Medicines Agency, 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=L02BB06) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/darolutamide/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/darolutamide/